Document Detail


Formulation of an intravenous emulsion loaded with a clarithromycin-phospholipid complex and its pharmacokinetics in rats.
MedLine Citation:
PMID:  18835427     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The purpose of this paper is to prepare a new formulation of clarithromycin emulsion (ClaE) with the clarithromycin-phospholipid complex which was analyzed by DSC. High-pressure homogenization, Nicomp 380 Particle Sizing system, and HPLC were used to prepare and investigate ClaE, while UPLC/MS/MS for pharmacokinetic study. Clarithromycin and soybean lecithin were reacted in dehydrated alcohol at a ratio of 1:10 for 3 h at 65 degrees C to prepare the complex. The ClaE formulation consisted of, according to quality percentage, the complex (clarithromycin 0.25% in ClaE), LCT 4%, MCT 16%, soybean lecithin 1.0%, F68 0.2%, Tween80 0.2%, glycerol 2.5%, sodium oleate 0.1% and L-cysteine 0.02%. ClaE was sterilized in a 100 degrees C revolving water bath for 30 min. The drug content, particle size distribution and entrapment efficiency of ClaE before and after sterilization and over 6 months storage at 10 degrees C were almost unchanged, while zeta-potential increased from -20.32 mV to -23.71 mV. These results show that ClaE has enough physicochemical stability to undergo sterilization and storage. The pharmacokinetic study showed that both ClaE and ClaS fitted a three-compartment model, their pharmacokinetic curves were similar and the main parameters showed no significant difference except Vss. ClaE has a great potential for clinical applications and industrial-scale production.
Authors:
Yan Lu; Yu Zhang; Ziyi Yang; Xing Tang
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Publication Detail:
Type:  Journal Article     Date:  2008-09-16
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  366     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2009 Jan 
Date Detail:
Created Date:  2008-12-29     Completed Date:  2009-04-07     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  160-9     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
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MeSH Terms
Descriptor/Qualifier:
Animals
Anti-Bacterial Agents / administration & dosage,  pharmacokinetics*
Chromatography, High Pressure Liquid
Clarithromycin / administration & dosage,  pharmacokinetics*
Drug Stability
Drug Storage
Emulsions
Excipients / chemistry*
Lecithins / chemistry*
Male
Particle Size
Rats
Rats, Wistar
Soybeans / chemistry
Sterilization
Tandem Mass Spectrometry
Chemical
Reg. No./Substance:
0/Anti-Bacterial Agents; 0/Emulsions; 0/Excipients; 0/Lecithins; 81103-11-9/Clarithromycin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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